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<p>Naproxen sodium (NaS) is employed to manage ocular inflammation and post-operative discomfort by inhibiting prostaglandin synthesis. However, achieving effective ocular bioavailability is challenging due insufficient drug retention and penetration. To address this challenge, the present study aims to formulate, and optimize NaS loaded eudragit nanoparticles (NaS-NPs) for improved ocular drug delivery and sustained release in the management of ocular inflammatory conditions. NaS-NPs were fabricated using double emulsion solvent evaporation technique by employing eudragit RL 100 (E-RL 100) and eudragit RS 100 (E-RS 100) polymers. The formulation was optimized by two-factor-three-level central composite design, where effect of concentration of polymer (E-RS100: E-RL100) and emulsifier (soya lecithin) on particle size, PDI, %EE, and drug release rate (%RR) was evaluated through response surface methodology to have sustained release formulation with maximum % EE and smaller particle size. The optimized batch of NaS nanoparticles (NaS-NPs<sub>opt</sub>) was further evaluated by FT-IR, DSC, <i>ex vivo</i> tolerance and permeation studies. The average particle size, PDI, %RR and %EE of all the batches of NaS-NPs were in range of 195–835&#xa0;nm, 0.215-1, 26.16–78.77% and 35.37–74.69% respectively. NaS-NPs<sub>opt</sub> exhibited 69.45% sustained <i>in vitro</i> release for 12&#xa0;h. Further, <i>ex vivo</i> studies revealed that NaS-NPs<sub>opt</sub> is non-irritant and exhibits approximately 1.71-fold higher corneal drug uptake compared to the drug solution. The study concludes that NaS-NPs were successfully developed and optimized, exhibiting sustained drug release and enhanced corneal drug permeation with no signs of ocular irritation, thus indicating their suitability as safe and effective systems for ocular drug delivery.</p> Graphical Abstract <p></p>

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Design, Optimization, and Evaluation of Naproxen Sodium Loaded Eudragit RL 100 and RS 100 Nanoparticles for Enhanced Ocular Drug Delivery

  • 期刊论文

  • 发表日期：

    2026年7月22日

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  • Gurpreet Kandav,
  • Deepika Modi

摘要

Naproxen sodium (NaS) is employed to manage ocular inflammation and post-operative discomfort by inhibiting prostaglandin synthesis. However, achieving effective ocular bioavailability is challenging due insufficient drug retention and penetration. To address this challenge, the present study aims to formulate, and optimize NaS loaded eudragit nanoparticles (NaS-NPs) for improved ocular drug delivery and sustained release in the management of ocular inflammatory conditions. NaS-NPs were fabricated using double emulsion solvent evaporation technique by employing eudragit RL 100 (E-RL 100) and eudragit RS 100 (E-RS 100) polymers. The formulation was optimized by two-factor-three-level central composite design, where effect of concentration of polymer (E-RS100: E-RL100) and emulsifier (soya lecithin) on particle size, PDI, %EE, and drug release rate (%RR) was evaluated through response surface methodology to have sustained release formulation with maximum % EE and smaller particle size. The optimized batch of NaS nanoparticles (NaS-NPsopt) was further evaluated by FT-IR, DSC, ex vivo tolerance and permeation studies. The average particle size, PDI, %RR and %EE of all the batches of NaS-NPs were in range of 195–835 nm, 0.215-1, 26.16–78.77% and 35.37–74.69% respectively. NaS-NPsopt exhibited 69.45% sustained in vitro release for 12 h. Further, ex vivo studies revealed that NaS-NPsopt is non-irritant and exhibits approximately 1.71-fold higher corneal drug uptake compared to the drug solution. The study concludes that NaS-NPs were successfully developed and optimized, exhibiting sustained drug release and enhanced corneal drug permeation with no signs of ocular irritation, thus indicating their suitability as safe and effective systems for ocular drug delivery.

Graphical Abstract